528201

PNU-120596

A urea derivative that acts as a potent, selective, and reversible positive allosteric modulator for the α7 subtype of neural nicotinic acetylcholine receptors

• Sinónimos: PNU-120596, α7 Neuronal Nicotinic Acetylcholine Receptor Agonist, PNU-120596, 1-(5-chloro-2,4-dimethoxy-phenyl)-3-(5-methyl-isoxazol-3-yl)-urea, a7 nAChR agonist, PNU-120596
• Fórmula empírica (notación de Hill): C₁₃H₁₄ClN₃O₄
• Número CAS: 501925-31-1
• Peso molecular: 311.72
• Número MDL: MFCD00095313
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥99% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: white
• solubilidad: DMSO: 100 mg/mL, clear, colorless
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• cadena SMILES: Clc1c(cc(c(c1)NC(=O)Nc2n[o]c(c2)C)OC)OC
• InChI: 1S/C13H14ClN3O4/c1-7-4-12(17-21-7)16-13(18)15-9-5-8(14)10(19-2)6-11(9)20-3/h4-6H,1-3H3,(H2,15,16,17,18)
• Clave InChI: CEIIEALEIHQDBX-UHFFFAOYSA-N

Descripción

Descripción general

A urea derivative that acts as a potent, selective, and reversible positive allosteric modulator for the α7 subtype of neural nicotinic acetylcholine receptors (EC₅₀ = 216 nM), with no significant effect on α4β2, α3β4 and α9α10 receptors. Specifically increase a-7 nAChR-mediated channel currents and channel mean open time in cultured neurons (~ 1 mM). However, it does neither affect ion selectivity nor unitary conductance. Shown to cross the blood-brain barrier. Causes conformational changes in the ligand binding domain of a7 nicotinic receptors that partially overlap with those caused by acetylcholine. Causes changes in cysteine accessibility at the inner beta sheet, transition zone, and agonist binding site. Also reported to potentiate agonist-evoked GABAergic postsynaptic inward currents in somatodendritic membrane of hippocampal interneurons.

Envase

Packaged under inert gas

Nota de preparación

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Hurst, R., et al. 2005. J. Neurosci. 25, 4396.
Barron, S., et al. 2009. Mol. Pharm.76, 253.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Cláusula de descargo de responsabilidad

Toxicity: Standard Handling (A)

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable